United States Patent (19) 11 Patent Number: 4,540,564 Bodor (45) Date of Patent: Sep
United States Patent (19) 11 Patent Number: 4,540,564 Bodor (45) Date of Patent: Sep. 10, 1985 54 BRAIN-SPECIFICDRUG DELIVERY 57 ABSTRACT 75 Inventor: Nicholas S. Bodor, Gainesville, Fla. The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug 73) Assignee: University of Florida, Gainesville, species to the brain, are: Fla. (a) compounds of the formula 21 Appl. No.: 516,382 22 Filed: Jul. 22, 1983 D-DHC) (I) Related U.S. Application Data wherein D is a centrally acting drug species, and 63 Continuation-in-part of Ser. No. 379,316, May 18, DHC is the reduced, biooxidizable, blood-brain 1982, Pat. No. 4,479,932, Ser. No. 461,543, Jan. 27, barrier penetrating lipoidal form of a dihydropyri 1983, , and Ser. No. 475,493, Mar. 15, 1983, , said Ser. dine - pyridinium salt redox carrier, with the No. 46,543, and Ser. No. 475,493, each is a continua proviso that when DHC) is tion-in-part of Ser. No. 379,316. 30 Foreign Application Priority Data O May 12, 1983 WO, PCT Int'l Appl. ......... WO83/00725 May 16, 1983 ICA) Canada ................................... 42892 51) Int. Cl...................... A61K 49/00; A61K 31/58; r’sN CO7J 17/00 52 U.S. Cl. ..................................... 424/9; 260/239.5; R 514/176 58 Field of Search .................. 424/9, 241; 260/239.5 wherein R is lower alkyl or benzyl and D is a drug species containing a single NH2 or OH func 56 References Cited tional group, the single OH group when present U.S.
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